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Compounds and methods for treatment of disorders associated with er stress

a technology of er stress and compounds, applied in the field of compounds and methods for treating disorders associated with er stress, can solve the problems of hypercholesterolemia, a growing health problem, and cholesterol-associated diseases becoming serious threats to human health, and achieve the effect of preventing complications

Inactive Publication Date: 2009-05-21
SYNDEXA PHARMA CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Hypercholesterolemia is a prevalent and growing health problem throughout the world.
These cholesterol-associated diseases have become serious threats to human health.

Method used

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  • Compounds and methods for treatment of disorders associated with er stress
  • Compounds and methods for treatment of disorders associated with er stress
  • Compounds and methods for treatment of disorders associated with er stress

Examples

Experimental program
Comparison scheme
Effect test

example 1

ERSE / URSE Activity Assay

[0369]The following assay may be used to identify compounds that will be useful in treating conditions related to ER stress.

[0370]When ER stress is triggered, a number of signaling events called unfolded protein response (UPR) is activated. One of the downstream effects of UPR is to increase transcriptional activity of genes with the promoter regions containing the endoplasmic reticulum stress element (ERSE) and unfolded response element (UPRE). One of UPR's eventual goals is to make more of those chaperone proteins needed for protein folding and destruction and thereby to increase functional capacity.

[0371]Accordingly, the compounds of the present invention may be analysed using this phenomena. For example, the results of screening test compounds may be expressed as percent induction of the ERSE reporter gene relative to tunicamycin treatment. Moreover, analysis may be made on ratios of reporter activity (firefly luciferase) / pCMV-RL (renilla luciferase) with...

example 2

[0391]

Soft Gelatin Capsule Formulation IItemIngredientsmg / Capsule1.Compound10.001-0.022.Butylated Hydroxytoluene (BHT)0.0163.Butylated Hydroxyanisole (BHA)0.0164.Miglyol 812 qs.160.0

Manufacturing Procedure:

[0392]1. BHT and BHA is suspended in Miglyol 812 and warmed to about 50° C. with stirring, until dissolved.

[0393]2. A compound of the invention is dissolved in the solution from step 1 at 50° C.

[0394]3. The solution from Step 2 is cooled at room temperature.

[0395]4. The solution from Step 3 is filled into soft gelatin capsules.

Note: All manufacturing steps are performed under a nitrogen atmosphere and protected from light.

example 3

[0396]

Soft Gelatin Capsule Formulation IIItemIngredientsmg / Capsule1.Compound of the invention10.001-0.022.di-α-Tocopherol0.0163.Miglyol 812 qs.160.0

Manufacturing Procedure:

[0397]1. Di-α-Tocopherol is suspended in Miglyol 812 and warmed to about 50° C. with stirring, until dissolved.

[0398]2. A compound of the invention.

[0399]3. The solution from Step 2 is cooled at room temperature.

[0400]4. The solution from Step 3 is filled into soft gelatin capsules.

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PUM

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Abstract

The invention provides novel compounds, methods for treating or preventing a condition related to ER-stress, e.g. hypercholesterolemia, atherosclerosis and related conditions, and pharmaceutical compositions related thereto.

Description

RELATED APPLICATIONS[0001]This application claims the benefit of priority to U.S. Provisional Application Nos. 60 / 785,328, 60 / 785,185, 60 / 785,154, 60 / 785,035, 60 / 785,007, 60 / 785,338, 60 / 785,182, 60 / 785,034, 60 / 785,335 and 60 / 785,235, all filed on Mar. 22, 2006. This application is related to the subject matter of U.S. patent application Ser. No. 11 / 227,497, filed Sep. 15, 2005, and U.S. patent application Ser. No. 11 / 227,543, filed Sep. 15, 2005. The contents of the aforementioned applications are each incorporated herein by reference, in their entireties.BACKGROUND OF THE INVENTION[0002]Obesity has been found to be associated with the activation of cellular stress signaling pathways (Uysal et al. Nature 389:610, 1997; Hirosumi et al. Nature 420:333, 2003; Yuan et al. Science 293:1673, 2001; each of which is incorporated herein by reference). One player in the cellular stress response is the endoplasmic reticulum (ER), a membranous network that functions in the synthesis and process...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/58C07J41/00C07D239/26C07C229/34A61K31/426A61K31/4409A61K31/13A61P9/10A61K31/195A61K31/495C07D277/30A61K31/575
CPCA61K9/4858A61P3/04A61P3/06A61P3/10A61P9/10A61P43/00C07J9/00
Inventor UYSAL, TEOMANCOSFORD, NICHOLAS D.P.
Owner SYNDEXA PHARMA CORP
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